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托美丁钠

托美丁钠用途

托美汀钠是一种口服有效的COX抑制剂,其IC50分别为0.35µM和0.82µM人COX-1和COX-2。托美汀钠是一种非甾体抗炎药(NSAID)[1][2]。

托美丁钠名称

[ CAS 号 ]:
35711-34-3

[ 中文名 ]:
痛灭定钠

[ 英文名 ]:
tolmetin sodium

[中文别名 ]:

[英文别名 ]:

托美丁钠生物活性

[ 描述 ]:

托美汀钠是一种口服有效的COX抑制剂,其IC50分别为0.35µM和0.82µM人COX-1和COX-2。托美汀钠是一种非甾体抗炎药(NSAID)[1][2]。

[ 相关类别 ]:

研究领域 >> 癌症
研究领域 >> 炎症/免疫
信号通路 >> 免疫及炎症 >> COX

[ 靶点 ]

Human COX-1:0.35 μM (IC50)

Human COX-2:0.82 μM (IC50)


[体外研究]

托美汀钠(0.25mM)不能减轻大鼠脑匀浆中的脂质过氧化。托美汀(0.25、0.5、0.75、1mM)具有清除自由基的特性,但在大鼠脑匀浆中不产生超氧阴离子[3]。托美汀钠(0.001-100μM)对HT-29结肠癌细胞系具有剂量依赖性的抗癌活性[4]。托美汀钠(0-100μM)对成骨细胞生长没有影响[5]。

[体内研究]

托美汀钠(30100mg/kg；灌胃；单剂量或每日两次,持续3天和14天)在单剂量后4小时显示出最大的溃疡形成作用,而在体重为180-200g的雄性Wistar大鼠中,重复给药3天后和14天后,其显著降低。托美汀以100mg/kg引起胃损伤[2]。托美汀钠(5 mg/kg,每天两次,共5天)预处理显著减轻喹啉酸(QA)诱导的神经毒性[3]。

[参考文献]

[1]. T D Warner, et al. Nonsteroid drug selectivities for cyclo-oxygenase-1 rather than cyclo-oxygenase-2 are associated with human gastrointestinal toxicity: a full in vitro analysis. Proc Natl Acad Sci U S A. 1999 Jun 22;96(13):7563-8.

[2]. Etcheverry SB, et al. Three new vanadyl(IV) complexes with non-steroidal anti-inflammatory drugs (Ibuprofen, Naproxen and Tolmetin). Bioactivity on osteoblast-like cells in culture. J Inorg Biochem. 2002 Jan 1;88(1):94-100.

[3]. DADAŞ, Yakup, et al. Synthesis and anticancer activity of some novel tolmetin thiosemicarbazides. Marmara Pharmaceutical Journal 19(3) • April 2015

托美丁钠物理化学性质

[ 密度 ]:
1.18g/cm3

[ 沸点 ]:
483.2ºC at 760 mmHg

[ 熔点 ]:
155-157ºC (DECOMPOSES)

[ 分子式 ]:
C15H14NNaO3

[ 分子量 ]:
279.26600

[ 闪点 ]:
246ºC

[ 精确质量 ]:
279.08700

[ PSA ]:
62.13000

[ LogP ]:
0.85690

托美丁钠毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :
UX9290000
CHEMICAL NAME :
1H-Pyrrole-2-acetic acid, 1-methyl-5-(p-toluoyl)-, sodium salt
CAS REGISTRY NUMBER :
35711-34-3
LAST UPDATED :
199504
DATA ITEMS CITED :
16
MOLECULAR FORMULA :
C14-H12-N-O3.Na
MOLECULAR WEIGHT :
265.26
WISWESSER LINE NOTATION :
T5MJ BVR D1& E1VO &-NA-

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Human - child
DOSE/DURATION :
2520 mg/kg/8W-I
TOXIC EFFECTS :
Blood - thrombocytopenia
REFERENCE :
ARHEAW Arthritis and Rheumatism. (Arthritis Foundation, 1314 Spring St., NW, Atlanta, GA 30309) V.1- 1958- Volume(issue)/page/year: 25,1144,1982
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Human - man
DOSE/DURATION :
538 mg/kg/61D-I
TOXIC EFFECTS :
Skin and Appendages - dermatitis, allergic (after systemic exposure)
REFERENCE :
JAMAAP JAMA, Journal of the American Medical Association. (AMA, 535 N. Dearborn St., Chicago, IL 60610) V.1- 1883- Volume(issue)/page/year: 243,1263,1980
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Human
DOSE/DURATION :
8 mg/kg
TOXIC EFFECTS :
Behavioral - hallucinations, distorted perceptions Vascular - BP lowering not characterized in autonomic section Vascular - shock
REFERENCE :
JAMAAP JAMA, Journal of the American Medical Association. (AMA, 535 N. Dearborn St., Chicago, IL 60610) V.1- 1883- Volume(issue)/page/year: 240,246,1978
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Human - woman
DOSE/DURATION :
8 mg/kg
TOXIC EFFECTS :
Spinal Cord - meningeal changes Sense Organs and Special Senses (Eye) - conjunctive irritation Liver - liver function tests impaired
REFERENCE :
JAMAAP JAMA, Journal of the American Medical Association. (AMA, 535 N. Dearborn St., Chicago, IL 60610) V.1- 1883- Volume(issue)/page/year: 245,67,1981
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
914 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
PBPSDY Pharmacological and Biochemical Properties of Drug Substances. (American Pharmaceutical Assoc., 2215 Constitution Ave., NW, Washington, DC 20037) V.1- 1977- Volume(issue)/page/year: 1,233,1977
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
770 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,532,1982
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
1050 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,532,1982
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
>724 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,532,1982
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
899 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
PBPSDY Pharmacological and Biochemical Properties of Drug Substances. (American Pharmaceutical Assoc., 2215 Constitution Ave., NW, Washington, DC 20037) V.1- 1977- Volume(issue)/page/year: 1,233,1977
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
690 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,532,1982
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
670 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,532,1982
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
>622 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,532,1982
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Mammal - dog
DOSE/DURATION :
>800 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
PBPSDY Pharmacological and Biochemical Properties of Drug Substances. (American Pharmaceutical Assoc., 2215 Constitution Ave., NW, Washington, DC 20037) V.1- 1977- Volume(issue)/page/year: 1,233,1977
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - hamster
DOSE/DURATION :
1584 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
PBPSDY Pharmacological and Biochemical Properties of Drug Substances. (American Pharmaceutical Assoc., 2215 Constitution Ave., NW, Washington, DC 20037) V.1- 1977- Volume(issue)/page/year: 1,233,1977 ** REPRODUCTIVE DATA **
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
100 mg/kg
SEX/DURATION :
female 1 day(s) pre-mating
TOXIC EFFECTS :
Reproductive - Fertility - other measures of fertility
REFERENCE :
FESTAS Fertility and Sterility. (American Fertility Soc., 608 13th Ave. S, Birmingham, AL 35282) V.1- 1950- Volume(issue)/page/year: 38,238,1982 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X5369 No. of Facilities: 53 (estimated) No. of Industries: 1 No. of Occupations: 1 No. of Employees: 2069 (estimated) No. of Female Employees: 1109 (estimated)

托美丁钠安全信息

[ 海关编码 ]:
2933990090

托美丁钠合成路线

详细合成路线

托美丁钠海关

[ 海关编码 ]: 2933990090

[ 中文概述 ]:
2933990090. 其他仅含氮杂原子的杂环化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:20.0%

[ 申报要素 ]: 品名, 成分含量, 用途, 乌洛托品请注明外观, 6－己内酰胺请注明外观, 签约日期

[ Summary ]:
2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

推荐生产厂家/供应商：

公司名：上海化源世纪贸易有限公司

区域：上海市普陀区

价格：

联系人：徐经理

产品详情：Tolmetin sodium

公司名：武汉鼎信通药业有限公司

区域：武汉市江夏区

价格：
￥需询单/1kg $需询单/10kg $需询单/50kg $需询单/500kg

联系人：董浩

产品详情：托美丁钠

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相关化合物

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